title: Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions.
abstract: We synthesized stapled helical leucine-based peptides (DPI-01-07) containing 2-aminoisobutyric acid and a covalent cross-linked unit as inhibitors of vitamin D receptor (VDR)-coactivator interactions. The effects of these peptides on the human VDR were examined in an inhibition assay based on the receptor cofactor assay system, and one of them, DPI-07, exhibited potent inhibitory activity (IC₅₀: 3.2 μM).
authors.affiliation: Division of Organic Chemistry, National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya, Tokyo 158-8501, Japan. demizu@nihs.go.jp
authors.forename: Yosuke
authors.initials: Y
authors.lastname: Demizu
authors.forename: Saori
authors.initials: S
authors.lastname: Nagoya
authors.forename: Manami
authors.initials: M
authors.lastname: Shirakawa
authors.forename: Megumi
authors.initials: M
authors.lastname: Kawamura
authors.forename: Nanako
authors.initials: N
authors.lastname: Yamagata
authors.forename: Yukiko
authors.initials: Y
authors.lastname: Sato
authors.forename: Mitsunobu
authors.initials: M
authors.lastname: Doi
authors.forename: Masaaki
authors.initials: M
authors.lastname: Kurihara
mesh_terms: D000621:Aminoisobutyric Acids / Q000737:chemistry; D001665:Binding Sites; D002942:Circular Dichroism; D030562:Databases, Protein; D006801:Humans; D051958:Nuclear Receptor Coactivator 2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D060066:Protein Interaction Maps / Q000187:drug effects; D017433:Protein Structure, Secondary; D017434:Protein Structure, Tertiary; D018167:Receptors, Calcitriol / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D000621:Aminoisobutyric Acids; D051958:Nuclear Receptor Coactivator 2; D010455:Peptides; D018167:Receptors, Calcitriol; C100049:2-aminoisobutyric acid